The synthesis, anti-inflammatory and antioxidant properties of novel 5-hydroxy-7-methyl-3H-thiazolo[4,5-b]pyridin-2-one derivatives were discussed. Fused thiazolo[4,5-b]pyridin-2-ones were synthesized and modified at the N3, C5 and C6 positions of the main core in order to obtain the compounds with a satisfactory pharmacological profile. The synthesized compounds were preselected via molecular docking for further testing of their anti-inflammatory activity in vitro. Evaluation of novel compounds over the carageenin induced rat paw edema revealed strong anti-inflammatory action of some compounds including (thiazolo[4,5-b]pyridin-3(2H)-yl) propanenitrile (5) and thiazolo[4,5-b]pyridin-3(2H)-yl) propanoic acid (6) even exceeding the standard - Ibuprofen. The antioxidant activity of the synthesized compounds was measured in vitro by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals.

Download full-text PDF

Source

Publication Analysis

Top Keywords

molecular docking
8
properties novel
8
synthesized compounds
8
compounds
5
synthesis molecular
4
docking biological
4
biological properties
4
novel thiazolo[45-b]pyridine
4
thiazolo[45-b]pyridine derivatives
4
derivatives synthesis
4

Similar Publications

In addressing the formidable challenge posed by methicillin-resistant Staphylococcus aureus (MRSA), this investigation elucidates a novel therapeutic paradigm by specifically targeting the virulence factor sortase A (SrtA) utilizing Tubuloside A (TnA). SrtA plays a critical role in the pathogenicity of MRSA, primarily by anchoring surface proteins to the bacterial cell wall, which is crucial for the bacterium's ability to colonize and infect host tissues. By inhibiting SrtA, TnA offers a novel and distinct strategy compared to traditional antibiotics.

View Article and Find Full Text PDF

Development of a novel multi-epitope subunit mRNA vaccine candidate to combat Acinetobacter baumannii.

Sci Rep

January 2025

Department of Respiratory Medicine, National Key Clinical Specialty, Branch of National Clinical Research Center for Respiratory Disease, Xiangya Hospital, Central South University, Changsha, 410008, Hunan, China.

Acinetobacter baumannii, an opportunistic bacterium prevalent in various environment, is a significant cause of nosocomial infections in ICUs. As the causative agent of pneumonia, septicemia, and meningitis, A. baumannii typically exhibits multidrug resistance and is associated with poor prognosis, thus led to a challenge for researchers in developing new treatment and prevention methods.

View Article and Find Full Text PDF

Network pharmacology uncovers that secoisolariciresinol diglucoside ameliorate premature ovarian insufficiency via PI3K/Akt pathway.

Sci Rep

January 2025

School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, No.461 Bayi Road, Donghu District, Nanchang, 330006, Jiangxi Province, People's Republic of China.

As one of the essential lignan derivative found in traditional Chinese medicinal herbs, secoisolariciresinol diglucoside (SDG) was proved to promote women's health through its phytoestrogenic properties. Increasingly studies indicated that this compound could be a potential drug capable of preventing estrogen-related diseases. Here, we aimed to investigate whether SDG can counteract cyclophosphamide (CTX) induced premature ovarian insufficiency (POI) and further explore its specific molecular mechanism.

View Article and Find Full Text PDF

In Silico-Guided Discovery of Polysaccharide Derivatives as Adjuvants in Nanoparticle Vaccines for Cancer Immunotherapy.

ACS Nano

January 2025

National Glycoengineering Research Center, Shandong Key Laboratory of Carbohydrate Chemistry and Glycobiology, NMPA Key Laboratory for Quality Research and Evaluation of Carbohydrate-Based Medicine, Shandong University, Qingdao 266237, China.

Cancer vaccines utilizing nanoparticle (NP) structures that integrate antigens and adjuvants to enhance delivery and stimulate immune responses are emerging as a promising avenue in cancer immunotherapy. However, the development of cancer vaccines has been significantly hindered by the low immunogenicity of tumor antigens. To address this challenge, substantial efforts have been made in developing innovative adjuvants to elicit effective immune responses.

View Article and Find Full Text PDF

GAS41 promotes ITGA4-mediated PI3K/Akt/mTOR signaling pathway and glioma tumorigenesis.

Biochem Pharmacol

January 2025

Bethune Institute of Epigenetic Medicine, The First Hospital of Jilin University, Changchun, Jilin 130021, China; International Center of Future Science, Jilin University, Changchun, 130012, China. Electronic address:

Glioma Amplified Sequence 41 (GAS41) is a chromatin-associated protein that belongs to the YEATS domain family of proteins and is frequently amplified in various tumors. However, its biological function and carcinogenic mechanism in gliomas are not fully understood. In this study, we revealed that GAS41 was upregulated in human glioma tissues and cell lines, and higher expression of GAS41 was significantly associated with poor clinical prognosis.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!